Riles Linda, Shaw Randal J, Johnston Mark, Reines Daniel
Department of Genetics, Washington University Medical School, St. Louis, MO, USA.
Yeast. 2004 Feb;21(3):241-8. doi: 10.1002/yea.1068.
Mutations in several genes encoding components of the RNA polymerase II elongation machinery render S. cerevisiae cells sensitive to the drug 6-azauracil (6AU), an inhibitor of IMP dehydrogenase and orotidylate decarboxylase. It is thought that a reduction in nucleotide levels following drug treatment causes transcriptional elongation to be more dependent on a fully functional RNA polymerase. To gain insight into the basis of the 6AU-sensitive phenotype and discern its specificity, we screened almost 3000 deletion mutants for growth in the presence of drug; 42 (1.5%) were reproducibly sensitive to the drug. The sensitive mutants included several missing known transcription elongation factors, but the majority were in genes involved in other cellular processes. Not all of the 6AU-sensitive strains displayed cross-sensitivity to mycophenolic acid (MPA), another drug that inhibits IMP dehydrogenase and has been employed as a screening agent for elongation mutants, showing that these two drugs are mechanistically distinct. Several of the mutants were tested for the ability to induce transcription of IMP dehydrogenase-encoding genes, in response to 6-AU and MPA treatment. As expected, mutants defective in transcriptional elongation factors were unable to fully induce IMPDH expression. However, most of the 6AU-sensitive strains had normal levels of IMPDH expression. Thus, although 6AU-sensitivity often results from defects in the elongation machinery, mutations that compromise processes other than transcription and induction of IMPDH also lead to sensitivity to this drug.
编码RNA聚合酶II延伸机制组成部分的几个基因发生突变,会使酿酒酵母细胞对药物6-氮尿嘧啶(6AU)敏感,6-氮尿嘧啶是肌苷酸脱氢酶和乳清酸脱羧酶的抑制剂。据认为,药物处理后核苷酸水平的降低会导致转录延伸更依赖于功能完全正常的RNA聚合酶。为了深入了解6AU敏感表型的基础并辨别其特异性,我们筛选了近3000个缺失突变体,以检测它们在药物存在下的生长情况;42个(1.5%)对该药物具有可重复性敏感性。敏感突变体包括几个缺失已知转录延伸因子的突变体,但大多数位于参与其他细胞过程的基因中。并非所有对6AU敏感的菌株都对霉酚酸(MPA)表现出交叉敏感性,MPA是另一种抑制肌苷酸脱氢酶的药物,已被用作延伸突变体的筛选剂,这表明这两种药物在机制上是不同的。测试了几个突变体在6-AU和MPA处理后诱导编码肌苷酸脱氢酶基因转录的能力。正如预期的那样,转录延伸因子有缺陷的突变体无法完全诱导IMPDH表达。然而,大多数对6AU敏感的菌株IMPDH表达水平正常。因此,虽然6AU敏感性通常源于延伸机制的缺陷,但损害转录和IMPDH诱导以外过程的突变也会导致对这种药物的敏感性。